LY404187

LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors. It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons. LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Cay-25330) in mouse and rat, respectively, models of Parkinson's disease when administered at a dose of 0.5 mg/kg per day.Formal Name: N-[2-(4'-cyano[1,1'-biphenyl]-4-yl)propyl]-2-propanesulfonamide. CAS Number: 211311-95-4. Molecular Formula: C19H22N2O2S. Formula Weight: 342.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 15mg/mL, DMSO: 15mg/mL, DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL, Ethanol: 3mg/mL. lambdamax: 278 nm. SMILES: CC(CNS(C(C)C)(=O)=O)C(C=C1)=CC=C1C2=CC=C(C#N)C=C2. InChi Code: InChI=1S/C19H22N2O2S/c1-14(2)24(22,23)21-13-15(3)17-8-10-19(11-9-17)18-6-4-16(12-20)5-7-18/h4-11,14-15,21H,13H2,1-3H3. InChi Key: HOQAVGZLYRYHSO-UHFFFAOYSA-N.